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说明： Potent colony-stimulating factor 1 receptor (CSF-1R) tyroine kinase inhibitor
化学名： 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide
纯度： ≥98% (HPLC)
生物活性 for Masitinib
Masitinib is a potent inhibitor of the tyrosine kinase receptor colony-stimulating factor 1R (CSF-1R) (IC50 = 90 nM). It is also an NLRP3 inflammasome activator. Masitinib additionally inhibits the proteolytic activity of SARS-CoV-2 main protease (Mpro) and blocks viral replication, as well as acting as a PDGFRα/β inhibitor. In vivo, Masitinib ameliorates cognitive impairment in transgenic mice model of Alzheimer's disease, and slows disease progression in a rat model of amyotrophic lateral sclerosis (ALS). Orally bioavailable.
技术数据 for Masitinib
| 分子量 | 498.64 |
| 公式 | C28H30N6OS |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 790299-79-5 |
| PubChem ID | 10074640 |
| InChI Key | WJEOLQLKVOPQFV-UHFFFAOYSA-N |
| Smiles | O=C(NC1=CC=C(C(=C1)NC2=NC(=CS2)C=3C=NC=CC3)C)C4=CC=C(C=C4)CN5CCN(C)CC5 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Masitinib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 49.86 | 100 | |
| ethanol | 4.99 | 10 |
制备储备液 for Masitinib
以下数据基于产品分子量 498.64。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.01 mL | 10.03 mL | 20.05 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.01 mL |
| 10 mM | 0.2 mL | 1 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for Masitinib
参考文献 for Masitinib
参考文献是支持产品生物活性的出版物。
Martínez-Ortega et al (2021) In silico characterization of Masitinib interaction with SARS-CoV-2 main protease. ChemMedChem. 16 2339 PMID: 34142459
Li et al (2020) Effects of chronic Masitinib treatment in APPswe/PSEN1dE9 transgenic mice modeling Alzheimer's disease. J.Alzheimers.Dis. 76 1339 PMID: 32623401
Trias et al (2016) Post-paralysis tyrosine kinase inhibition with masitinib abrogates neuroinflammation and slows disease progression in inherited amyotrophic lateral sclerosis. J.Neuroinflammation 13 177 PMID: 27400786
Ettcheto et al (2021) Masitinib for the treatment of Alzheimer's disease. Neurodegener.Dis.Manag. 11 263 PMID: 34412534
Drayman et al (2021) Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. Science 373 931 PMID: 34285133
If you know of a relevant reference for Masitinib, please let us know.
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关键词: Masitinib, Masitinib supplier, potent, CSF-1R, NLRP3, inflammasome, activator, SARS-CoV-2, Mpro, Alzheimer, disease, AD, amyotrophic, lateral, sclerosis, ALS, orally, bioavailable, in, vivo, PDGFR, Other, RTKs, Inflammasomes, 3C, and, 3CL, Proteases, Coronavirus, 7705, Tocris Bioscience
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